JP2016504990A - Ｂｅｔタンパク質抑制性ジヒドロピリドピラジノン - Google Patents

Ｂｅｔタンパク質抑制性ジヒドロピリドピラジノン Download PDF

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Publication number
JP2016504990A
JP2016504990A JP2015548421A JP2015548421A JP2016504990A JP 2016504990 A JP2016504990 A JP 2016504990A JP 2015548421 A JP2015548421 A JP 2015548421A JP 2015548421 A JP2015548421 A JP 2015548421A JP 2016504990 A JP2016504990 A JP 2016504990A
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Japan
Prior art keywords
amino
dimethyl
oxo
pyrazin
tetrahydropyrido
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Ceased
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JP2015548421A
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English (en)
Japanese (ja)
Inventor
シユメーズ，ノルベルト
バーダー，ベンヤミン
ヘンドラー，ベルナルト
シユテツキト，デトレフ
レヨイネ，パスカレ
フエルナンデズ−モンタルバン，アマウリー・エルネスト
シユテルフエルト，テイモ
ガレンカンプ，ダニエル
Original Assignee
バイエル ファーマ アクチエンゲゼルシャフト
バイエル ファーマ アクチエンゲゼルシャフト
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Publication of JP2016504990A publication Critical patent/JP2016504990A/ja
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2015548421A 2012-12-20 2013-12-17 Ｂｅｔタンパク質抑制性ジヒドロピリドピラジノン Ceased JP2016504990A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP12198623 2012-12-20
EP12198623.6 2012-12-20
EP13182252.0 2013-08-29
EP13182252 2013-08-29
EP13191933 2013-11-07
EP13191933.4 2013-11-07
PCT/EP2013/076784 WO2014095774A1 (fr) 2012-12-20 2013-12-17 Dihydropyridopyrazinones inhibitrices de protéine bet

Publications (1)

Publication Number Publication Date
JP2016504990A true JP2016504990A (ja) 2016-02-18

Family

ID=49779903

Family Applications (1)

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JP2015548421A Ceased JP2016504990A (ja) 2012-12-20 2013-12-17 Ｂｅｔタンパク質抑制性ジヒドロピリドピラジノン

Country Status (10)

Country Link
US (1) US20160193206A1 (fr)
EP (1) EP2935260A1 (fr)
JP (1) JP2016504990A (fr)
CN (1) CN105229002A (fr)
AR (1) AR094148A1 (fr)
CA (1) CA2895404A1 (fr)
HK (1) HK1213899A1 (fr)
TW (1) TW201427981A (fr)
UY (1) UY35205A (fr)
WO (1) WO2014095774A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017512186A (ja) * 2014-01-31 2017-05-18 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジヒドロプテリジノン誘導体およびその使用
US10730860B2 (en) 2014-01-31 2020-08-04 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
US10793571B2 (en) 2014-01-31 2020-10-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
US10881668B2 (en) 2015-09-11 2021-01-05 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof
US10913752B2 (en) 2015-11-25 2021-02-09 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
US11306105B2 (en) 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160193206A1 (en) * 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
CA2917562A1 (fr) * 2013-07-09 2015-01-15 Bayer Pharma Aktiengesellschaft Dihydroquinoxalinones et dihydropyridopyrazinones inhibitrices de proteine bet modifiees
WO2015013635A2 (fr) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibiteurs des facteurs de transcription et leurs utilisations
WO2015081203A1 (fr) 2013-11-26 2015-06-04 Incyte Corporation Hétérocycles bicycliques servant d'inhibiteurs des protéines bet
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (fr) 2013-12-19 2015-06-25 Incyte Corporation Hétérocycles tricycliques en tant qu'inhibiteurs des protéines bet
HUE061770T2 (hu) 2014-04-23 2023-08-28 Incyte Holdings Corp 1H-pirrolo[2,3-C]piridin-7(6H)-onok és pirazolo[3,4-C]piridin-7(6H)-onok mint BET fehérjék gátlószerei
CN106573931A (zh) * 2014-06-18 2017-04-19 拜耳医药股份有限公司 抑制BET蛋白的具有间位取代的芳族氨基或醚基的3，4‑二氢吡啶并[2，3‑b]吡嗪酮
WO2015193217A1 (fr) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Dérivés de dihydropyrido[2,3-b]pyrazinone inhibant la protéine bet, à groupe éther ou amino aromatique para-substitué
KR102633122B1 (ko) 2014-08-01 2024-02-05 누에볼루션 에이/에스 브로모도메인에 대하여 활성을 갖는 화합물
JP2017525759A (ja) * 2014-08-08 2017-09-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジヒドロプテリジノン誘導体およびその使用
RU2017104897A (ru) 2014-08-08 2018-09-10 Дана-Фарбер Кэнсер Инститьют, Инк. Производные диазепана и их применения
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
JP6930913B2 (ja) 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US10501438B2 (en) 2015-08-11 2019-12-10 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024406A1 (fr) * 2015-08-11 2017-02-16 Neomed Institute Lactames bicycliques n-substitués, leur préparation et leur utilisation en tant qu'agents pharmaceutiques
EP3334719B1 (fr) 2015-08-12 2021-09-15 Neomed Institute Benzimidazoles substitués, préparation et utilisation de ceux-ci en tant qu'agents pharmaceutiques
WO2017066876A1 (fr) 2015-10-21 2017-04-27 Neomed Institute Imidazopyridines substituées, leur préparation et leur utilisation comme médicaments
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
EP3472157B1 (fr) 2016-06-20 2023-04-12 Incyte Corporation Formes cristallines solides d'un inhibiteur bet
CN109350616B (zh) * 2018-12-18 2020-04-21 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法
WO2023205251A1 (fr) 2022-04-19 2023-10-26 Nuevolution A/S Composés actifs vis-à-vis de bromodomaines

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19506742A1 (de) * 1995-02-27 1996-08-29 Bayer Ag Verwendung von Chinoxalinen in Kombination mit Protease-Inhibitoren als Arzneimittel zur Behandlung von AIDS und/oder HIV-Infektionen
US7351709B2 (en) * 2004-06-09 2008-04-01 Wyeth Estrogen receptor ligands
EP2078016B1 (fr) * 2006-10-19 2012-02-01 Signal Pharmaceuticals LLC Composés hétéroaryle, compositions de ceux-ci et procédés de traitement avec ceux-ci
JP2012197231A (ja) * 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体
CA2799373A1 (fr) * 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions et procedes permettant de moduler un metabolisme
US20160193206A1 (en) * 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017512186A (ja) * 2014-01-31 2017-05-18 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジヒドロプテリジノン誘導体およびその使用
US10730860B2 (en) 2014-01-31 2020-08-04 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
US10793571B2 (en) 2014-01-31 2020-10-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
US10881668B2 (en) 2015-09-11 2021-01-05 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof
US11306105B2 (en) 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
US11406645B2 (en) 2015-09-11 2022-08-09 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof
US10913752B2 (en) 2015-11-25 2021-02-09 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof

Also Published As

Publication number Publication date
US20160193206A1 (en) 2016-07-07
EP2935260A1 (fr) 2015-10-28
WO2014095774A1 (fr) 2014-06-26
TW201427981A (zh) 2014-07-16
AR094148A1 (es) 2015-07-15
HK1213899A1 (zh) 2016-07-15
CN105229002A (zh) 2016-01-06
UY35205A (es) 2014-07-31
CA2895404A1 (fr) 2014-06-26

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